ABSTRACT
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In the last decade, combinatorial chemistry has become a versatile and powerful tool for
generating libraries of new chemical entities for the pharmaceutical industry. Meanwhile,
biocatalytic methods have developed and provided complementary approaches and in some
cases powerful alternatives to conventional synthetic chemical techniques, due to their high
chemo-, regio-, and stereoselectivity. Moreover, the ability of enzyme or microbial catalysis to
perform difficult chemical reactions, such as hydroxylations of nonactivated carbons, on
structurally complex molecules, without the need of protection/deprotection steps of reactive
functional groups, was recognized. That promoted new strategies for the use of biocatalysis as
an additional tool for the multiple modification of synthetic or natural products [1], and the
development of a biocombinatorial chemistry (‘‘combinatorial biocatalysis’’) for generating
molecular diversity, as a novel approach in drug discovery and development [2-4].
